Heptares Therapeutics, the leading GPCR drug discovery and development company,
announces the publication of a new paper describing how 'reverse pharmacology', enabled
by its StaR(R) technology, can be applied to and accelerate GPCR-based drug discovery.
The paper has been published in Molecular Pharmacology (ref. 1) and is available online
by clicking here

The authors from Heptares describe for the first time how StaR technology enables
the study of isolated GPCRs locked in conformations that correspond to agonist or
antagonist pharmacology, and the elucidation of their respective 3D structures.

These StaRs and structures can be used to select and design compounds with specific
pharmacologies, such as inverse agonist, partial agonist or full agonist, based on their
ability to bind differentially to the agonist and antagonist StaRs. For example a full
agonist will preferentially bind to the agonist StaR.

This approach is termed 'reverse pharmacology' since classically compounds are made
and tested in cells and tissues, and only then can their preferred receptor conformation
and activity be determined, a process subject to variation depending on the assay system
and lacking precision.

"The ability to predict whether a compound will behave as an agonist, inverse
agonist or antagonist in an in vitro, in silico or in vivo setting is a very powerful
tool for drug discovery," said Fiona Marshall, Heptares' Chief Scientific Officer.
"Combining this approach with our unique StaR technology is enabling Heptares to advance
our pipeline of novel compounds targeting important GPCR targets, and those of our
partners, towards the clinic."